New aporphinoid 5-HT2A and α1A antagonists via structural manipulations of nantenine.
Bioorg Med Chem
; 19(19): 5861-8, 2011 Oct 01.
Article
em En
| MEDLINE
| ID: mdl-21900013
ABSTRACT
A series of C1, C2, C3 and N6 analogs of nantenine (2) was synthesized and evaluated in 5-HT(2A) and α(1A) receptor functional assays. Alkyl substitution of the C1 and N6 methyl groups of nantenine provided selective 5-HT(2A) and α(1A) antagonists, respectively. The C2 alkyloxy analogs studied were generally selective for α(1A) versus 5-HT(2A). The C3 bromo analog 15 is one of the most potent aporphinoid 5-HT(2A) antagonists known presently.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Aporfinas
/
Receptores Adrenérgicos alfa 1
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Receptor 5-HT2A de Serotonina
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Antagonistas de Receptores Adrenérgicos alfa 1
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Antagonistas do Receptor 5-HT2 de Serotonina
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article